A novel strategy for the synthesis of enzymatically stable biotin–DOTA conjugates for in vivo use

Abstract

Two ¹¹¹In radiolabelled biotin–DOTA conjugates were prepared containing an enzymatically stable amine bond (–CH₂–NH–CH₂–). Syntheses are straightforward and molecules were labelled with high radiochemical purity. They were also found to be stable in human plasma. This strategy provides a method to produce a simple biotin derivative not requiring any additional protection groups against biotinidase.